US20030031711A1 - Method of treating gastroesophageal reflux disease and nocturnal acid breakthrough - Google Patents

Method of treating gastroesophageal reflux disease and nocturnal acid breakthrough Download PDF

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US20030031711A1
US20030031711A1 US10/152,914 US15291402A US2003031711A1 US 20030031711 A1 US20030031711 A1 US 20030031711A1 US 15291402 A US15291402 A US 15291402A US 2003031711 A1 US2003031711 A1 US 2003031711A1
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administered
dosage
dosage form
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John Fara
Bret Berner
Verne Cowles
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Assertio Therapeutics Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/009—Sachets, pouches characterised by the material or function of the envelope
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0065—Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants

Definitions

  • the present invention relates to the use of GABA B receptor agonists, and in particular baclofen (4-amino-3-(4-chlorophenyl)butanoic acid) for the concurrent treatment of gastroesophageal reflux disease and nocturnal acid breakthrough.
  • Gastroesophageal reflux disease may be caused by a variety of mechanisms, which include transient lower esophageal sphincter relaxations (“TLESRs”), decreased lower esophageal sphincter resting tone, impaired esophageal acid clearance, delayed gastric emptying, decreased salivation and impaired tissue resistance.
  • TLESRs transient lower esophageal sphincter relaxations
  • impaired esophageal acid clearance typically occur during the early daytime hours, but some GERD sufferers also experience reflux during the night, even when being treated with proton pump inhibitors.
  • These nighttime episodes of reflux are referred to as nocturnal acid breakthrough (“NAB”).
  • NAB is defined as a nocturnal gastric pH less than 4 for greater than 1 hour.
  • baclofen has been extensively studied, both for its therapeutic applications and the various means by which the agent could be administered. For example, numerous studies have been conducted on the use of baclofen for the treatment of chronic hiccups, an affliction that often occurs in conjunction with gastroesophageal disease. See for example, Gueland, et al., European Respiratory Journal 8(2):235-237, 1995.
  • baclofen Another problem encountered with adminstering baclofen is that absorption of baclofen into the blood stream occurs only in the upper gastrointestinal tract. Therefore, extended release versions of the most commonly used dosage forms such as tablets, capsules, and liquid formulations are not suitable for delivery of baclofen to treat GERD and NAB.
  • drug delivery systems that are suitable for use in the method of treatment of the invention as they are particularly tailored to be gastric-retained dosages, such as those described in Sinnreich, U.S. Pat. No. 4,996,058; Franz, et al., U.S. Pat. No. 5,232,704; Wong, et al., U.S. Pat. No. 6,120,803; Shell, et al., U.S. Pat. No. 5,972,389; and Shell, et al., WO 9855107.
  • One aspect of the invention relates to a method of concurrently treating gastroesophageal reflux disease and nocturnal acid breakthrough comprising administering a therapeutically effective amount of a GABA B receptor agonist in the evening to a mammal in need of such treatment.
  • Another aspect of the invention pertains to a method of concurrently treating gastroesophageal reflux disease and nocturnal acid breakthrough comprising administering a therapeutically effective amount of 4-amino-3-(4-chlorophenyl) butanoic acid (“baclofen”), or a pharmaceutically acceptable salt or an optical isomer thereof in the evening to a mammal in need of such treatment.
  • baclofen 4-amino-3-(4-chlorophenyl) butanoic acid
  • Still yet another aspect of the invention relates to a method of concurrently treating gastroesophageal reflux disease and nocturnal acid breakthrough comprising administering a therapeutically effective amount of the R enantiomer of 4-amino-3-(4-chlorophenyl) butanoic acid in the evening to a mammal in need of such treatment.
  • Another aspect of the invention pertains to a method of concurrently treating gastroesophageal reflux disease and nocturnal acid breakthrough comprising administering a therapeutically effective amount a GABA B receptor agonist in the evening to a mammal in need of such treatment, in combination with a therapeutic agent selected from the group consisting of proton pump inhibitors and histamine H2-receptor blockers.
  • FIG. 1 illustrates plasma concentration of Baclofen following administration of 20-mg Baclofen as Lioresal®, the commercially available immediate release product, or Baclofen, extended release, a gastric retentive tablet.
  • FIG. 2 illustrates plasma concentration of Baclofen following administration of 20 mg Baclofen as Lioresal®, the commercially available immediate release product or a Baclofen EGTS, a gastric retentive drug delivery formulation.
  • the lower esophageal sphincter (“LES”) usually remains closed. However, when it relaxes at an inappropriate time, it allows acid and food particles to reflux into the esophagus. The process of secondary peristalsis returns most of the acid and food to the stomach and then the LES closes again. Any acid remaining in the esophagus is neutralized by saliva, and then is cleared into the stomach. Patients with GERD experience an increased number of transient LES relaxations and therefore, more frequent reflux episodes which increases the cumulative amount of time gastric acid spends in the esophagus. In addition, there are other factors that add to the increased esophageal acid exposure time that GERD patients experience, such as a decrease in the amplitude of secondary peristaltic waves which results in less effective esophageal acid clearance.
  • GERD patients experience more than discomfort as the extent and severity of esophageal mucosal injury worsens.
  • the associated pathological conditions include a variety of esophageal disorders such as erythema, isolated, confluent and circumferential erosions, deep ulcers, esophageal stricture and replacement of normal esophageal epithelium with abnormal (Barrett's) epithelium, which is a precancerous condition.
  • Patients may also experience pain (odynophagia) or difficulty in swallowing (dysphagia); pulmonary symptoms such as chronic coughing, wheezing, asthma, aspiration pneumonia, and interstitial fibrosis; oral symptoms such as tooth enamel decay, gingivitis and halitosis; throat symptoms such as a soreness, laryngitis, hoarseness, and a globus sensation; and earache.
  • the instant invention is a method of concurrently treating gastroesophageal reflux disease and nocturnal acid breakthrough comprising administering to a mammal in need of such treatment a therapeutically effective amount of a GABA B receptor agonist.
  • treating covers treating the disease of GERD and NAB in a mammal, particularly a human, and includes:
  • the method comprises administering a therapeutically effective amount of 4-amino-3-(4-chlorophenyl)butanoic acid (“baclofen”), or a pharmaceutically acceptable salt or an optical isomer thereof.
  • baclofen 4-amino-3-(4-chlorophenyl)butanoic acid
  • R enantiomer of 4-amino-3-(4-chlorophenyl) butanoic acid is administered.
  • the invention also contemplates administering one or more additional therapeutic agents with the GABA B receptor agonist treatment.
  • additional therapeutic agents are selected from the group consisting of proton pump inhibitors and histamine H2-receptor blockers.
  • GABA B receptor agonists suitable for use in the methods of the invention. These include by way of illustration and not limitation, ⁇ -amino- ⁇ -(p-halophenyl)-butyric acids and their esters (Keberle, et al., U.S. Pat. No. 3,471,548), as well as the pharmaceutically acceptable salts or optical isomers thereof.
  • substituted aminopropyl acid derivatives described in Andrews, et al., U.S. Pat. No. 6,117,908. These include by way of illustration and not limitation: 4-aminobutanoic acid; 4-amino-3-(4-chlorophenyl) butanoic acid (baclofen); 4-amino-3-phenylbutanoic acid; 4-amino-3-hydroxybutanoic acid; 4-amino-3-(4-chlorophenyl)-3-hydroxyphenylbutanoic acid; 4-amino-3-(thien-2-yl) butanoic acid; 4-amino-3-(5-chlorothien-2-yl) butanoic acid; 4-amino-3-(5-bromothien-2-yl) butanoic acid; 4-amino-3-(5-methylthien-2-yl) butanoic acid; 4-amino-3-(2-imidazolyl) butanoi
  • a particularly useful GABA B receptor agonist is the ⁇ -amino- ⁇ -(p-halophenyl)-butyric acid referred to as 4-amino-3-(4-chlorophenyl) butanoic acid (“baclofen”).
  • the methods of the invention also contemplate the addition of one or more therapeutic agents with the GABA B receptor agonist treatment.
  • additional therapeutic agents are selected from the group consisting of proton pump inhibitors and histamine H2-receptor blockers.
  • Proton pump inhibitors act by inhibiting gastric acid secretion.
  • proton pump inhibitors that can be used in the methods of the invention include, by way of illustration and not limitation, omeprazole, lansoprazole, pantoprazole, rabeprazole and esomeprazole.
  • Histamine H2-receptor blockers are administered to both prevent and relieve reflux symptoms such as heartburn, acid indigestion and sour stomach as well as being used to treat duodenal ulcers and prevent their return. Histamine H2-receptor blockers act by inhibiting histamine stimulation of the gastric parietal cell and thereby suppress gastric acid secretion. Examples of histamine H2-receptor blockers that can be used in the methods of the invention include, by way of illustration and not limitation, cimetidine and cimetidine HCl, famotidine, nizatidine, ranitidine and ranitidine HCl, and other suitable salts.
  • Pharmaceutically acceptable salts of the agonist or the additional therapeutic agent(s) can also be used in the methods of the invention as long as the salt form retains the biological effectiveness and properties of the agonist or the additional therapeutic agent(s), and are not biologically or otherwise undesirable.
  • Such pharmaceutically acceptable salts may be amphoteric and may be present in the form of internal salts.
  • the agonist and other agents may form acid addition salts and salts with bases.
  • Exemplary acids that can be used to form such salts include, by way of example and not limitation, mineral acids such as hydrochloric, hydrobromic, sulfuric or phosphoric acid or organic acids such as organic sulfonic acids and organic carboxylic acids.
  • Salts formed with inorganic bases include, for example, the sodium, potassium, lithium, ammonium, calcium, and magnesium salts.
  • Salts derived from organic bases include, for example, the salts of primary, secondary and tertiary amines, substituted amines including naturally-occurring substituted amines, and cyclic amines, including isopropylamine, trimethylamine, diethylamine, triethylamine, tripropylamine, ethanolamine, 2-dimethyl aminoethanol, tromethamine, lysine, arginine, histidine, caffeine, procaine, hydrabamine, choline, betaine, ethylenediamine, glucosamine, N-alkylglucamines, theobromine, purines, piperazine, piperidine, N-ethylpiperidine, fumarate, maleate, succinate, acetate and oxalate.
  • Optical isomers can also be used in the methods of the invention.
  • the agonist baclofen is a chiral compound due to the presence of an asymmetric carbon atom.
  • baclofen may be administered in the form of mixtures of isomers (e.g., racemates), or in the form of pure isomers (e.g., enantiomers).
  • GABA B receptor agonist and “therapeutic agent” are intended to include the compounds themselves as well as their pharmaceutically acceptable salts and optical isomers.
  • the term “therapeutically effective amount” refers to that amount which is sufficient to effect treatment, when administered to a mammal in need of such treatment.
  • the therapeutically effective amount will vary depending on the subject being treated, the severity of the disease state and the manner of administration, and may be determined routinely by one of ordinary skill in the art.
  • GABA B receptor agonists such as baclofen may be used at doses appropriate for other conditions for which other GABA B receptor agonists have been administered.
  • the method of the invention will involve administering the GABA B receptor agonist on a daily basis for as long as the conditions (GERD and NAB) persist.
  • An effective dosage is typically in the range of about 5-100 mg/dosage, typically about 10-80 mg/dosage, more typically about 20-60 mg/dosage.
  • the dosage is typically in the range of about 15-100 mg/dosage, typically about 15-80 mg/dosage, more typically about 15-60 mg/dosage.
  • the dosage is typically in the range of about 20-800 mg/dosage, typically about 20-500 mg/dosage, more typically about 20-400 mg/dosage.
  • a GABA B receptor agonist is administered in the evening, for example, with the evening meal or near bedtime.
  • the method of administering a GABA B receptor agonist in the evening further includes administering an additional therapeutic agent simultaneously with the administration of the GABA B receptor agonist, said agent being selected from the group consisting of proton pump inhibitors, histamine H2-receptor blockers and combinations thereof.
  • an additional therapeutic agent simultaneously with the administration of the GABA B receptor agonist, said agent being selected from the group consisting of proton pump inhibitors, histamine H2-receptor blockers and combinations thereof.
  • the term “simultaneous” is intended to mean administration of the agonist and additional agent at approximately the same time, i.e., in the evening and therefore includes administration together and administration of the agonist and agent within a few hours of each other.
  • the method of administering a GABA B receptor agonist in the evening further includes administering an additional therapeutic agent in the daytime, where the additional agent is selected from the group consisting of GABA B receptor agonists, proton pump inhibitors, histamine H2-receptor blockers and combinations thereof. Typically this additional agent would be administered in the morning, for example with breakfast.
  • the method of administering a GABA B receptor agonist in the evening further includes administering an additional therapeutic agent simultaneously with the administration of the GABA B receptor agonist and administering an additional therapeutic agent in the daytime.
  • One exemplary therapeutic regimen is administering a smaller dose of a GABA B receptor agonist in the morning, followed by a larger dose of an GABA B receptor agonist in the evening, where the smaller dosage in the morning also serves to minimize any sedation effects.
  • Another exemplary therapeutic regimen is administering a proton pump inhibitor or histamine H2-receptor blocker in the morning, followed by administering an GABA B receptor agonist in the evening, where the evening dosage optionally includes a proton pump inhibitor or histamine H2-receptor blocker.
  • a typical dosage form would provide for a drug delivery profile such that the agonist is delivered for a period of at least 6 hours.
  • the evening dosage form of the GABA B receptor agonist is a film coated dosage form or a capsule dosage form that allows for the extended release of the GABA B receptor agonist in the stomach and comprises: (a) at least one component that expands on contact with gastric juice and contains an agent capable of releasing carbon dioxide or nitrogen, a GABA B receptor agonist; (b) at least one hydrophilic membrane in the form of a sachet which contains component (a), expands by inflation, floats on the aqueous phase in the stomach and is permeable to gastric juice and; (c) a film coating or capsule form which contains components (a) and (b) and which disintegrates without delay in the stomach under the action of gastric juice.
  • Component (a) may also contain a pharmaceutically acceptable hydrophilic swelling agent such as lower alkyl ethers of cellulose, starches, water-soluble aliphatic or cyclic poly-N-vinylamides, polyvinyl alcohols, polyacrylates, polymethacrylates, polyethylene glycols and mixtures thereof, as well as other materials used in the manufacture of pharmaceutical dosage forms. Further details regarding an example of this type of dosage form can be found in Sinnreich, U.S. Pat. No. 4,996,058.
  • the evening dosage form of the GABA B receptor agonist is an extended release oral drug dosage form for releasing the GABA B receptor agonist into the stomach, duodenum and small intestine of a patient, and comprises: a plurality of solid particles consisting of the GABA B receptor agonist dispersed within a polymer that (i) swells unrestrained dimensionally by imbibing water from gastric fluid to increase the size of the particles to promote gastric retention in the stomach of the patient in which the fed mode has been induced; (ii) gradually the drug diffuses or the polymer erodes over a time period of hours, where the diffusion or erosion commences upon contact with the gastric fluid; and (iii) releases the agonist to the stomach, duodenum and small intestine of the patient, as a result of the diffusion or polymeric erosion at a rate corresponding to the time period.
  • Exemplary polymers include polyethylene oxides, alkyl substituted cellulose materials and combinations thereof, for example, high molecular weight polyethylene oxides and high molecular weight or viscosity hydroxypropylmethylcellulose materials. Further details regarding an example of this type of dosage form can be found in Shell, et al., U.S. Pat. No. 5,972,389 and Shell, et al., WO 9855107.
  • a bi-layer tablet releases the GABA B receptor agonist to the upper gastrointestinal tract from an active containing layer, while the other layer is a buoyant or floating layer. Details of this dosage may be found in Franz, et al., U.S. Pat. No. 5,232,704.
  • the dosage form of the present invention may be surrounded by a band of insoluble material as described by Wong, et al., U.S. Pat. No. 6,120,803.
  • the evening dosage form of the GABA B receptor agonist is a pharmaceutical composition in the form of an adhesive tablet, and comprises a hydrophobic tablet core, the top surface of which adheres to the receptor surface of the oral mucosa, and which consists of the GABA B receptor agonist.
  • the tablet may contain excipients such as a swellable vinyl polymer, a galactomannan, a wax, a glyceride, a completely hydrogenated glyceride and a partially hydrogenated glyceride.
  • the tablet may have a hydrophobic coating which covers the tablet core with the exception of the surface provided for the release of the GABA B receptor agonist. Further details regarding this dosage form can be found in Khanna, et al., U.S. Pat. No. 5,091,184.
  • the GABA B receptor agonist is delivered systemically through the skin throughout the day and night as a transdermal patch, as described in Mazzenga, et al., U.S. Pat. No. 5,073,539.
  • the proton pump inhibitor or histamine H2-receptor blocker can either be administered in a dosage form that includes the GABA B receptor agonist or can be administered in a dosage form that is separate from the GABA B receptor agonist. Exemplary dosage forms are described below.
  • the daytime dosage can be any suitable formulation as are well known in the art.
  • the method of the invention includes administering a GABA B receptor agonist, proton pump inhibitor or histamine H2-receptor blocker in the morning, with the GABA B receptor agonist being delivered in the evening, then there are numerous commercially available dosage forms that can be administered.
  • other formulations can be readily designed based upon knowledge in the art, and include the gastric-retained delivery systems described above.
  • Typical dosage forms of the proton pump inhibitor suitable for use in the invention include capsules and tablets.
  • One of skill in the art can readily prepare one of these exemplary formulations or the proton pump inhibitor can be administered by means of one of the numerous commercially available products, which include, for example, Prilosec® (omeprazole, AstraZenca), Prevacid® (lansoprazole, TAP Pharmaceutical Products, Inc.), Protonix® (pantoprazole, Wyeth-Ayerst Laboratories) and Aciphex® (rabeprazole, Eisan, Inc.).
  • Prilosec® omeprazole, AstraZenca
  • Prevacid® lansoprazole, TAP Pharmaceutical Products, Inc.
  • Protonix® pantoprazole, Wyeth-Ayerst Laboratories
  • Aciphex® rabeprazole, Eisan, Inc.
  • Typical dosage forms of the histamine H2-receptor blocker suitable for use in the invention include syrups, solutions, suspensions, tablets (including chewable and oral disintegrating tablets), capsules, and effervescent formulations of granules or tablets.
  • One of skill in the art can readily prepare one of these exemplary formulations or the histamine H2-receptor blocker can be administered by means of one of the numerous commercially available products, which include, for example, Tagamet® (cimetidine, GlaxoSmithKline), Pepcid® (famotidine, Merck & Co.), Axid® (nizatidine, Eli Lilly & Co.) and Zantac® (ranitidine, Pfizer).
  • dosage forms typically contain the active agent (GABA B receptor agonist, proton pump inhibitor or histamine H2-receptor blocker) in combination with one or more pharmaceutically acceptable ingredients.
  • the carrier may be in the form of a solid, semi-solid or liquid diluent, or a capsule.
  • the amount of active agent is about 0.1-95 wt %, more typically about 1-50 wt %.
  • Actual methods of preparing such dosage forms are known, or will be apparent, to those skilled in this art; for example, see Remington's Pharmaceutical Sciences, Mack Publishing Company, Easton, Pa., 18th Edition, 1990.
  • the dosage form to be administered will, in any event, contain a quantity of the additional therapeutic agent(s) in an amount effective to alleviate the symptoms of the subject being treated.
  • the agent may be mixed with solid, powdered ingredients, such as lactose, saccharose, sorbitol, mannitol, starch, amylopectin, cellulose derivatives, gelatin, or another suitable ingredient, as well as with disintegrating agents and lubricating agents such as magnesium stearate, calcium stearate, sodium stearyl fumarate and polyethylene glycol waxes.
  • solid, powdered ingredients such as lactose, saccharose, sorbitol, mannitol, starch, amylopectin, cellulose derivatives, gelatin, or another suitable ingredient
  • disintegrating agents and lubricating agents such as magnesium stearate, calcium stearate, sodium stearyl fumarate and polyethylene glycol waxes.
  • Soft gelatin capsules may be prepared by mixing the active agent and vegetable oil, fat, or other suitable vehicle.
  • Hard gelatin capsules may contain granules of the active agent, alone or in combination with solid powdered ingredients such as lactose, saccharose, sorbitol, mannitol, potato starch, corn starch, amylopectin, cellulose derivatives or gelatin.
  • Liquid preparations for oral administration may be prepared in the form of syrups or suspensions, e.g. solutions or suspensions containing about 0.2-20 wt % of the active agent and the remainder consisting of sugar or sugar alcohols and a mixture of ethanol, water, glycerol, propylene glycol and polyethylene glycol. If desired, such liquid preparations may contain coloring agents, flavoring agents, saccharin and carboxymethyl cellulose or other thickening agents. Liquid preparations for oral administration may also be prepared in the form of a dry powder to be reconstituted with a suitable solvent prior to use.
  • Tablets from Example 2 were made with an Amberlite® ion exchange resin containing 1 MBq of 111 Indium.
  • the tablets were administered to 4 healthy volunteers after a low fat breakfast and visualized by gamma scintigraphy.
  • Blood samples were taken at specified intervals and analyzed for Baclofen concentration in the plasma and compared to plasma concentration in the same subjects after administration of the immediate release baclofen tablet, Lioresal® 20-mg.
  • FIG. 1 illustrates plasma concentration of Baclofen following administration of 20-mg Baclofen as Lioresal®, the commercially available immediate release product, or Baclofen, extended release, a gastric retentive tablet.
  • FIG. 1 and Table 1 demonstrate the expected extended release attributes with a lower maximum concentration and later time of maximum concentration as compared to the immediate release product.
  • FIG. 2 illustrates plasma concentration of Baclofen following administration of 20 mg baclofen as Lioresal®, the commercially available immediate release product or a Baclofen EGTS, a gastric retentive drug delivery formulation.
  • FIG. 2 and Table 2 demonstrate the expected extended release attributes with a lower maximum concentration and later time of maximum concentration as compared to the immediate release product.
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MXPA03011096A (es) 2004-12-06
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